Information on EC 3.5.1.98 - histone deacetylase

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The expected taxonomic range for this enzyme is: Bacteria, Eukaryota

EC NUMBER
COMMENTARY hide
3.5.1.98
-
RECOMMENDED NAME
GeneOntology No.
histone deacetylase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
hydrolysis of an N6-acetyl-lysine residue of a histone to yield a deacetylated histone
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
deacetylation
hydrolysis
SYSTEMATIC NAME
IUBMB Comments
histone amidohydrolase
A class of enzymes that remove acetyl groups from N6-acetyl-lysine residues on a histone. The reaction of this enzyme is opposite to that of EC 2.3.1.48, histone acetyltransferase. Histone deacetylases (HDACs) can be organized into three classes, HDAC1, HDAC2 and HDAC3, depending on sequence similarity and domain organization. Histone acetylation plays an important role in regulation of gene expression. In eukaryotes, HDACs play a key role in the regulation of transcription and cell proliferation [4]. May be identical to EC 3.5.1.17, acyl-lysine deacylase.
CAS REGISTRY NUMBER
COMMENTARY hide
9076-57-7
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
i.e. Bordetella sp. strain FB188
SwissProt
Manually annotated by BRENDA team
Alcaligenes sp. DSM 11172
i.e. Bordetella sp. strain FB188
SwissProt
Manually annotated by BRENDA team
isoform AtHD1
Uniprot
Manually annotated by BRENDA team
isozyme HDAC3
-
-
Manually annotated by BRENDA team
-
Uniprot
Manually annotated by BRENDA team
isoform Hda-7, class II enzyme
-
-
Manually annotated by BRENDA team
Candida albicans ATCC 90028
gene HOS2
-
-
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
isoform dHDAC1, i.e. dRPD3
-
-
Manually annotated by BRENDA team
variety Minghui63
-
-
Manually annotated by BRENDA team
variety Zhonghua11
UniProt
Manually annotated by BRENDA team
strain GK24
-
-
Manually annotated by BRENDA team
strain GK24
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
isoforms HD1B-I, HD1B-II
Uniprot
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
Set3C is a conserved nuclear complex, Set3 interacts with Hos2
malfunction
metabolism
-
nitrative/oxidative stress reduce HDAC2 expression via nitration of distinct tyrosine residues. Peroxynitrite, hydrogen peroxide and cigarette smoke-conditioned medium reduce HDAC2 expression in A549 epithelial cells in vitro. This reduction is due to increased proteasomal degradation following ubiquitination rather than reduction of mRNA expression or stability
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
AC-Arg-Gly-Lys(AC)-4-amino-7-methylcoumarin + H2O
?
show the reaction diagram
-
substrate activity assay
-
-
?
Ac-DQK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-FEK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-GGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-GS(PO3)K(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-GSK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-IHK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-ILK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-KGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-KSK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-KWK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-KYK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin + H2O
Ac-Leu-Gly-Lys-7-amido-4-methylcoumarin + acetate
show the reaction diagram
-
-
-
?
Ac-LIK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-LYK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-PFK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-VLK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-GAK(acetyl)-7-amido-4-methylcoumarin + H2O
acetyl-GAK-7-amino-4-methylcoumarin + acetate
show the reaction diagram
-
-
-
-
?
acetyl-tubulin + H2O
tubulin + acetate
show the reaction diagram
-
major HDAC6 substrate
-
-
?
acetylated histone + H2O
acetate + histone
show the reaction diagram
-
-
-
-
?
alpha-Tubulin + H2O
?
show the reaction diagram
-
splicing variant HDAC6p114 is intact in its deacetylase activity against a-tubulin
-
-
?
alpha-tubulin + H2O
acetate + ?
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + acetate
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + trifluoroacetate
show the reaction diagram
-
-
-
-
?
Boc-acetyl-Lys-7-amido-4-methylcoumarin + H2O
Boc-acetyl-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
Boc-trifluoroacetyl-Lys-7-amido-4-methylcoumarin + H2O
Boc-trifluoroacetyl-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Fluor de Lys + H2O
?
show the reaction diagram
Fluor de Lys H4-AcK16 + H2O
?
show the reaction diagram
-
-
-
-
?
Fluor de Lys HDAC substrate + H2O
?
show the reaction diagram
Fluor de Lys HDAC8 substrate + H2O
?
show the reaction diagram
N-acetyl-arginine-histidine-acetyl-lysine-acetyl-lysine-coumarin + H2O
?
show the reaction diagram
-
substrate in crystallized enzyme-substrate complex
-
-
?
N-acetyl-Lys16-histone H4 + H2O
acetate + histone H4
show the reaction diagram
-
-
-
?
N-acetyl-lysine-alpha-tubulin + H2O
acetate + alpha-tubulin
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-heat shock protein 90 + H2O
acetate + heat shock protein 90
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-histone + H2O
acetate + histone
show the reaction diagram
N-acetyl-lysine-histone H1 + H2O
acetate + histone H1
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-histone H3 + H2O
acetate + histone H3
show the reaction diagram
N-acetyl-lysine-histone H3 + H2O
histone H3 + acetate
show the reaction diagram
-
deacetylation occurs at Lys9 and Lys23
-
-
?
N-acetyl-lysine-histone H4 + H2O
acetate + histone H4
show the reaction diagram
N-acetyl-lysine-MyoD + H2O
acetate + MyoD
show the reaction diagram
N-acetyl-lysine4-histone H3 + H2O
acetate + histone H3
show the reaction diagram
-
-
-
-
?
N6-lysine acetylated histone H2A + H2O
histone H2A + acetate
show the reaction diagram
-
substrate of isoforms HDAC1, HDAC2, HDAC. Isoform HDAC3 preferentially cleeaves lysines 5 H2A
-
-
?
N6-lysine acetylated histone H2A-H2B dimer + H2O
histone H3-H4 dimer + acetate
show the reaction diagram
N6-lysine acetylated histone H3 + H2O
histone H3 + acetate
show the reaction diagram
N6-lysine acetylated histone H3-H4 tetramer + H2O
histone H3-H4 tetramer + acetate
show the reaction diagram
N6-lysine acetylated histone H4 + H2O
histone H4 + acetate
show the reaction diagram
N6-lysine acetylated histone H4 peptide + H2O
histone H4 peptide + acetate
show the reaction diagram
peptide of N-terminal 20 amino acids
-
-
?
N6-lysine-acetylated histone H4 peptide + H2O
acetate + histone H4 peptide
show the reaction diagram
-
-
-
?
RHK(acetyl)K(acetyl)-fluorophore + H2O
RHKK-fluorophore + acetate
show the reaction diagram
tert-butyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + acetate
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
alpha-Tubulin + H2O
?
show the reaction diagram
-
splicing variant HDAC6p114 is intact in its deacetylase activity against a-tubulin
-
-
?
alpha-tubulin + H2O
acetate + ?
show the reaction diagram
-
-
-
-
?
N-acetyl-Lys16-histone H4 + H2O
acetate + histone H4
show the reaction diagram
P70288
-
-
-
?
N-acetyl-lysine-alpha-tubulin + H2O
acetate + alpha-tubulin
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-heat shock protein 90 + H2O
acetate + heat shock protein 90
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-histone + H2O
acetate + histone
show the reaction diagram
N-acetyl-lysine-histone H1 + H2O
acetate + histone H1
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-histone H3 + H2O
acetate + histone H3
show the reaction diagram
-
-
-
-
?
N-acetyl-lysine-histone H4 + H2O
acetate + histone H4
show the reaction diagram
N-acetyl-lysine-MyoD + H2O
acetate + MyoD
show the reaction diagram
-
transcription factor MyoD, its activity is co-dependent on isoform HDAC1 and transcriptional co-activator P/CAF
-
-
?
N-acetyl-lysine4-histone H3 + H2O
acetate + histone H3
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ATP
-
required for deacetylation of histone H4 in purified nucleosomes by isoforms HDAC1 and HDAC3. ATP also enhances cleavage of free, non-nucleosomal histones by HDAC1 and HDAC3
additional information
-
deacetylation by isoform dHDAC1 does not require any additional cofactors
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
Zn2+, Mg2+, or Mn2+ is required. Zn2+ is the most efficient
Na+
-
Na+ binds more weakly to both monovalent cation sites and activates HDAC8 to a lesser extent than K+
Ni2+
-
ratio of kcat to KM value in presence of metal ion in decreasing order: Co(II), Fe(II), Zn(II), Ni(II)
Zinc
-
enzyme active site consists of a tubular pocket, a zinc-binding site and two D-H charge-relay systems
additional information
-
the identity of the catalytic metal ion influences both the Michaelis-Menten constant and the affinity of inhibitor suberoylanilide hydroxamic acid, with Fe(II) and Co(II) giving KM values 5fold lower than that of Zn(II). Apo-enzyme has a low residual level of activity
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2E)-3-[1,2-bis(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-benzyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-benzyl-2-(2-phenylethyl)-1H-benzimidazol-6-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-ethyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[2-(diethylamino)ethyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[3-(dimethylamino)-2,2-dimethylpropyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[3-(dimethylamino)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[4-(dimethylamino)butyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[2-cyclohexyl-1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[2-[(benzyloxy)methyl]-1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[4-([[2-(3a,7a-dihydro-1H-indol-3-yl)ethyl](2-hydroxyethyl)amino]methyl)phenyl]-N-hydroxyprop-2-enamide
-
-
(2E)-N-(2-aminophenyl)-3-(4-{1-[(2-hydroxyethyl)amino]-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl}phenyl)prop-2-enamide
(2E)-N-(2-aminophenyl)-3-(4-{1-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl}phenyl)prop-2-enamide
(2E)-N-(2-aminophenyl)-3-[2-(2-phenylethyl)-1-(pyridin-2-ylmethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-(2-aminophenyl)-3-[4-(1-{[2-(morpholin-4-yl)ethyl]amino}-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl)phenyl]prop-2-enamide
(2E)-N-(2-aminophenyl)-3-{4-[2-(4-bromoanilino)-1-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]phenyl}prop-2-enamide
(2E)-N-hydroxy-3-naphthalen-1-ylprop-2-enamide
-
HDAC8-selective inhibitor
(2E)-N-hydroxy-3-[1-(2-morpholin-4-ylethyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(1-methylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-methylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-phenylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-octyl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-thiophen-3-yl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-methoxypropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-morpholin-4-ylpropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-methyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-[3-(1H-imidazol-1-yl)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-[3-(2-oxopyrrolidin-1-yl)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(2-piperidin-1-ylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(2-pyrrolidin-1-ylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(3,4,5-trimethoxybenzyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(3-pyrrolidin-1-ylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(pyridin-2-ylmethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-propyl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-[(4-methoxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.93 microM
(2E)-N-hydroxy-3-[2-[2-(1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.22 microM
(2E)-N-hydroxy-3-[2-[2-(2-methyl-1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.1042microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation
(2E)-N-hydroxy-3-[2-[2-(pyrazolo[1,5-a]pyridin-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.53 microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation
(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
-
(2S)-2-(acetylamino)-3-[3-[(2S)-2-[[(2S)-2-ammonio-7-(hydroxyamino)-7-oxoheptanoyl]amino]-3-methoxy-3-oxopropyl]phenyl]propanoate
-
-
(2S)-8-oxo-2-[(3-piperidin-1-ylpropanoyl)amino]-N-quinolin-3-ylnonanamide
-
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]-2-fluorophenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-benzyl-N-(4-chlorophenyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(3-methylphenyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(4-methylphenyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(6-methylpyridin-3-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(piperidin-1-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(propan-2-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-2-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-3-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-4-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-phenylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-[4-(propan-2-yl)phenyl]pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-[4-(trifluoromethyl)phenyl]pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2,4-difluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2-chloro-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3,4-dichlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3,4-difluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-bromo-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-chloro-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-methoxyphenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-bromophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chloro-3-methylphenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2,2-trifluoroethyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2-difluoroethyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2-dimethylpropyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-fluoroethyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-hydroxy-2-methylpropyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-hydroxyethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-methoxyethyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(3-hydroxy-2,2-dimethylpropyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(cyanomethyl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(propan-2-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(pyrimidin-2-yl)pyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-cyclobutylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-ethylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-cyanophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-cyclopropylphenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-fluoro-3-methylphenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-methoxyphenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(5-chloropyridin-2-yl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-cyclopentyl-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-cyclopropyl-1-methylpyrrolidine-3-carboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N~3~-(4-chlorophenyl)-N~1~,N~1~-diethylpyrrolidine-1,3-dicarboxamide
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N~3~-(4-chlorophenyl)-N~1~-ethylpyrrolidine-1,3-dicarboxamide
(3R)-4-{5-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyrazin-2-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{5-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridin-2-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{6-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridazin-3-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R)-4-{6-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridin-3-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3R,4S)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
(3S)-3-{[(3S)-3-{[(benzyloxy)carbonyl]amino}-3-cyclopropylpropanoyl]amino}-2-oxo-5-phenylpentyl acetate
-
-
(3S,15R,20aS)-15-methyl-3-[(1E)-4-sulfanylbut-1-en-1-yl]-3,4,6,7,14,15,18,19,20,20a-decahydro-1H,5H,16H-11,8:15,12-di(azeno)pyrrolo[2,1-c][1,8,12,4,15]oxadithiadiazacyclooctadecine-1,5,16-trione
-
(3S,6S,10S,14S)-3-(1H-indol-3-ylmethyl)-10-methyl-14-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,11-tetraazacyclotetradecane-2,5,8,12-tetrone
-
-
(3S,6S,9S,13S)-3-(1H-indol-3-ylmethyl)-9,10-dimethyl-13-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
-
(3S,6S,9S,13S)-3-(1H-indol-3-ylmethyl)-9-methyl-13-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
-
(3S,6S,9S,15aS)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-3-(6-oxooctyl)decahydro-1H-pyrrolo[1,2-a][1,4,7,10]tetraazacyclotridecine-1,4,7,11(8H)-tetrone
-
-
(4E)-N-(2-aminophenyl)-5-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]pent-4-enamide
-
(4Z)-6-[(5R,8S,11R)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-4-enoic acid
-
(5E)-N-(2-aminophenyl)-6-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-5-enamide
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3-thia-7,14,20,21-tetraazatricyclo[14.3.1.1-2,5]henicosa-1(20),2(21),16,18-tetraene-6,9,13-trione
-
(5R,8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8R,11R)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8S,11S,5'S,8'S,11'S)-11,11'-[disulfanediyldi(1E)but-1-ene-4,1-diyl]bis[5-methyl-8-(1-methylethyl)-3,10,17-trioxa-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione]
-
(8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),4,16(19)-tetraene-6,9,13-trione
-
(E)-3-[3-[4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl]phenyl]-N-hydroxyacrylamide
-
inhibitor for both EGFR/HER2 kinase and HDAC with potent cellular activity, i.e. target inhibition and cytotoxicity
(E)-N1-hydroxy-N5-(5-styryl-1,3,4-thiadiazol-2-yl)glutaramide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0059 and 0.00675 microM, respectively
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-(naphthalen-1-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-m-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-o-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-p-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-pentyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-phenethyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-phenyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride
-
-
(S)-benzyl 3-(biphenyl-4-ylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-benzyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenethylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-benzyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-N-(2,4-dimethylphenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-(3-chloro-4-fluorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-(3-chlorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-(4-fluorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-(biphenyl-4-yl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-benzyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride
-
-
(S)-N-hexyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-N-tert -butyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
-
(S)-tert-butyl 3-(2,4-dimethylphenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(3-chloro-4-fluorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(3-chlorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(4-fluorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(benzylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(biphenyl-4-ylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(hexylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 3-(tert-butylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(4-methoxyphenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(mtolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(naphthalen-1-ylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(o-tolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(p-tolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(pentylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenethylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
-
1,10-phenanthroline
10 mM, 66% inhibition
1-methyl-N-[(1S)-7-oxo-1-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]octyl]piperidine-2-carboxamide
-
-
1-[5-(2,3-dihydro-1,4-benzodioxin-6-yl)thiophen-2-yl]-2,2,2-trifluoroethanone
-
-
1-[5-(4-acetylphenyl)thiophen-2-yl]-2,2,2-trifluoroethanone
-
-
15-deoxy-DELTA12,14-prostaglandin J2-biotin
-
maximal inhibition of recombinant HDAC3 in complex with CoR1 is 50%
2,2,2-trifluoro-1-(2-phenyl-1,3-thiazol-5-yl)ethanone
-
-
2,2,2-trifluoro-1-(4-phenylthiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-phenylthiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-[3-[(methylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
potent inhibitor of HDAC4 and shows more than 100fold selectivity overHDAC1
2,2,2-trifluoro-1-(5-[3-[(propylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-[3-[(thiophen-2-ylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-[5-(1H-indol-5-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(2-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(3-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(3-methyl-1,2,4-oxadiazol-5-yl)thiophen-2-yl]ethanone
-
HDAC4-selective inhibitor
2,2,2-trifluoro-1-[5-(3-[[(4-fluorobenzyl)sulfonyl]methyl]-1,2,4-oxadiazol-5-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(4-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(pyridin-2-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(quinoxalin-6-yl)thiophen-2-yl]ethanone
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide
-
competitive. Significant but rather unselective inhibition of cellular HDACs
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenylamide
2,3-dihydrobenzoic acid
-
98% residual activity at 0.5 mM
2-(3,6-dihydroxy-9H-xanthen-9-yl)25-(8-(hydroxyamino)28-oxooctanamido)benzoic acid
-
synthesis, overview
-
2-(3,6-dihydroxy-9H-xanthen-9-yl)25-(8-methoxy-8-oxooctanamido)benzoic acid
-
synthesis, overview
-
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
-
-
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
-
-
2-hydroxybutyric acid
-
96% residual activity at 0.5 mM
2-[(methylsulfonyl)sulfanyl]ethanaminium bromide
-
-
2-[(methylsulfonyl)sulfanyl]ethyl 2-propylpentanoate
-
-
3,4-Dihydroxyphenyl acetic acid
-
90% residual activity at 0.5 mM
3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide
-
APHA
3-benzoylbenzoic acid
-
and hydroxamate analogs
3-benzoylpropanoic acid
-
and hydroxamate analogs
3-hydroxycinnamic acid
-
96% residual activity at 0.5 mM
3-[5-(trifluoroacetyl)thiophen-2-yl]benzoic acid
-
the inhibitor shows 40fold selectivity for HDAC4 and 180fold for HDAC6 against HDAC1
3-[5-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]-2-(2-phenylethyl)-1H-benzimidazol-1-yl]propanoic acid
-
-
3-[5-[4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl]furan-2-yl]-N-hydroxy-acrylamide
-
inhibitor for both EGFR/HER2 kinase and HDAC with potent cellular activity, i.e. target inhibition and cytotoxicity
4-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl 2-propylpentanoate
-
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
-
M344
4-benzoylbutyric acid
-
and hydroxamate analogs
4-benzoylbutyric hydroxamic acid
-
-
4-hydroxy-2-nonenal
-
maximal inhibition of recombinant HDAC3 in complex with CoR1 is 70%
4-Phenylbutyric acid
-
and hydroxamate analogs
4-[5-(trifluoroacetyl)thiophen-2-yl]benzoic acid
-
-
4-[5-(trifluoroacetyl)thiophen-2-yl]benzonitrile
-
-
4-[[(2E)-2-(2-chlorobenzylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
-
-
4-[[(2E)-2-(4-chlorobenzylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
-
inactivates HDAC8 preferentially over HDAC1
4-[[(2E)-2-(anthracen-9-ylmethylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
-
-
5-(4-benzyl-1H-1,2,3-triazol-1-yl)-N-hydroxypentanamide
-
-
5-(4-hydroxyphenyl)-3H-1,2-dithiol-3-thione
-
-
5-phenylvaleric acid
-
and hydroxamate analogs
5-phenylvaleric hydroxamic acid
-
-
6-mercapto-N-phenylhexanamide
-
-
6-[(1-(mercaptomethyl)vinyl)amino]-N-phenylhexanamide
-
-
6-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
6-[(2E)-2-[(2-bromo-4-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
6-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
6-[(2S,5S,8S,11S)-8-(1H-indol-3-ylmethyl)-2-methyl-11-(2-methylpropyl)-3,6,9,13-tetraoxo-1,4,7,10-tetraazacyclotridecan-5-yl]hexanoic acid
-
-
6-[(9H-fluoren-3-ylmethyl)(3-phenoxybenzyl)amino]-N-hydroxyhexanamide
6-[(biphenyl-4-ylmethyl)[4-[(4-bromobenzyl)oxy]benzyl]amino]-N-hydroxyhexanamide
-
-
6-[4-(2,6-dimethoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-2-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-3-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[[4-[(4-bromobenzyl)oxy]benzyl](9H-fluoren-3-ylmethyl)amino]-N-hydroxyhexanamide
-
-
6-{4-[4-(dimethylamino)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyhexanamide
-
-
7-mercapto-N-(2-phenyl-1,3-thiazol-5-yl)heptanamide
-
-
7-mercapto-N-(3-phenoxyphenyl)heptanamide
-
-
7-mercapto-N-phenylheptanamide
-
thiol formed by enzymatic hydrolysis in the cell reacts with the zinc ion in the active site of histone deacetylase. Molecular modeling of complex with histone HDAC8
7-mercapto-N-pyridin-3-ylheptanamide
-
-
7-mercapto-N-quinolin-3-ylheptanamide
-
-
7-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(2-bromo-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(2-bromophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(2-bromopyridin-3-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(2-chlorophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[(2E)-2-[[4-(dimethylamino)-2-hydroxyphenyl]methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
7-[4-(biphenyl-3-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyheptanamide
-
-
7-{4-[4-(dimethylamino)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyheptanamide
-
-
8-hydroxyquinoline
-
85% residual activity at 0.5 mM
8-[(2E)-2-[(2,5-dihydroxyphenyl)methylidene]hydrazino]-N-hydroxy-8-oxooctanamide
-
acetylated histone deacetylase 1
-
the activity of HDAC2 is inhibited by acetylated HDAC1
-
allyl mercaptan
-
garlic organosulfur compounds can be metabolized to allyl mercaptan
alpha-keto-gamma-methylselenobutyrate
-
causes dose-dependent inhibition of HDAC activity, HDAC1 shows about 80% residual activity at 2 mM, HDAC8 shows less than 60% residual activity at 2 mM
apicidin
apicidin A
-
-
azumamide A
-
-
azumamide E
-
-
Baclofen
-
98% residual activity at 0.5 mM
belinostat
-
PXD101
beta-methylselenopyruvate
-
causes dose-dependent inhibition of HDAC activity, competitive inhibitor of HDAC8, HDAC1 shows about 30% residual activity at 2 mM, HDAC8 shows less than 30% residual activity at 2 mM
Butyrate
Butyric acid
caffeic acid
-
80% residual activity at 0.5 mM
chidamide
chlorogenic acid
-
highly potent HDAC inhibitor, 40% residual activity at 0.5 mM
Cinnamic acid
-
95% residual activity at 0.5 mM
curcumin
-
highly potent HDAC inhibitor, 52% residual activity at 0.5 mM
cyclo (N-O-methyl-L-tryptophanyl-L-isoleucinyl-D-pipecolinyl-L-2-amino-8-oxodecanoyl)
-
i.e. apicidin, a cyclic tetrapeptide having broad-spectrum antiparasitic activity, inhibits the enzyme activity as well as the in vitro growth of Babesia parasites with an IC50 of 3.8 ng/ml
-
D-(-)-quinic acid
-
96% residual activity at 0.5 mM
dihydrocaffeic acid
-
86% residual activity at 0.5 mM
EDTA
-
1 mM, 30 min, complete loss of activity. Zn2+, Mg2+, Mn2+ may restore activity
entinostat
ferulic acid
-
80% residual activity at 0.5 mM
FK-228
FK228
-
-
FOXP
-
FOXP3 specifically inhibits binding of histone deacetylase 2 and 4 to the site and increases local histone H3 acetylation
-
FR235222
-
-
FR901228
-
Gal4-dHDAC1, consisting of the N-terminal 147 amino acid residues of the yeast Gal4 protein fused to the N terminus of full-length dHDAC1 protein, but not dHDAC1, is able to repress transcription in vitro. Transcriptional repression is blocked by the enzyme inhibitor FR901228
FR901375
-
-
gamma-aminobutyric acid
-
-
HC-toxin
HDAC1 siRNA
-
-
-
indol-2-carboxylic acid
-
97% residual activity at 0.5 mM
isobutyric acid
-
80% residual activity at 0.5 mM
Isothiocyanate
-
found in cruciferous vegetables
ITF-2357
JNJ-26481585
-
broad-spectrum or pan-HDAC inhibitor
K+
-
K+ bound to monovalent cation site 1 inhibits catalytic activity of HDAC8 (11fold less active with two K+ ions bound compared to one K+ ion bound), partial inhibition at high KCl
LAQ-824
-
-
LAQ824
largazole
LBH-589
LBH589
Mandelic acid
-
85% residual activity at 0.5 mM
MC1568
specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs
MC1575
specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs; specificity for class II HDACs
MC1863
-
-
MCP30
-
30 kDa protein isolated from bitter melon seeds, Momordica charantia, contains two highly related type I ribosome-inactivating proteins, alpha- and beta-momorcharin
-
methyl (3R,6R,9R)-9-(acetylamino)-6-[6-(hydroxyamino)-6-oxohexyl]-5,8-dioxo-4,7-diazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3-carboxylate
-
tight binding competitive inhibition
methyl N-[(2S)-2-[(N-acetyl-L-alanyl)amino]-7-(hydroxyamino)-7-oxoheptanoyl]-L-phenylalaninate
-
-
MGCD 290
-
an enzyme Hos2 inhibitor, for use in combination with azoles, such as fluconazole, for fungal infections
-
MGCD-0103
mocetinostat
MS-275
N-(2-aminophenyl)-4-[[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]methyl]benzamide
-
-
N-(2-aminophenyl)-4-[[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]methyl]benzamide
-
-
N-(2-aminophenyl)-5-[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-aminophenyl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-aminophenyl)-6-(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(2-aminophenyl)-6-(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(2-aminopyridin-3-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-hydroxyphenyl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(4-aminopyrimidin-5-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(6-mercaptohexyl)-1-benzofuran-2-carboxamide
-
-
N-(6-mercaptohexyl)-1H-indole-2-carboxamide
-
-
N-(6-mercaptohexyl)-2-naphthamide
-
-
N-(6-mercaptohexyl)benzamide
-
-
N-(8-aminonaphthalen-1-yl)-5-[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(8-aminonaphthalen-1-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(8-aminonaphthalen-1-yl)-6-(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(8-aminonaphthalen-1-yl)-6-(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-biphenyl-3-yl-7-mercaptoheptanamide
-
-
N-hydroxy-1-(3-hydroxypropyl)-2-(2-phenylethyl)-1H-benzimidazole-5-carboxamide
-
-
N-hydroxy-1-methyl-indole-6-carboxamide
-
HDAC8-selective inhibitor
N-hydroxy-2-[1-methyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]cyclopropanecarboxamide
-
-
N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-methylpropyl)-1H-benzimidazol-5-yl]propanamide
-
-
N-hydroxy-3-[2-(2-phenylethyl)-1-(3,4,5-trimethoxybenzyl)-1H-benzimidazol-5-yl]propanamide
-
-
N-hydroxy-3-[2-[(2-methyl-1H-indol-3-yl)acetyl]-2,3-dihydro-1H-isoindol-5-yl]propanamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.19 microM
N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
-
N-hydroxy-4-[[(2E)-2-(2-hydroxybenzylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
-
inactivates HDAC8 preferentially over HDAC1
N-hydroxy-4-[[(2E)-2-(4-methylbenzylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
-
-
N-hydroxy-4-[[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
-
-
N-hydroxy-4-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}butanamide
N-hydroxy-5-(4-phenyl-1H-1,2,3-triazol-1-yl)pentanamide
-
-
N-hydroxy-5-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}pentanamide
N-hydroxy-6-(4-phenyl-1H-1,2,3-triazol-1-yl)hexanamide
-
-
N-hydroxy-6-[(2S,5S,8S,11S)-8-(1H-indol-3-ylmethyl)-2-methyl-11-(2-methylpropyl)-3,6,9,13-tetraoxo-1,4,7,10-tetraazacyclotridecan-5-yl]hexanamide
-
-
N-hydroxy-6-[(3S,6S,9S,15aS)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-1,4,7,11-tetraoxotetradecahydro-1H-pyrrolo[1,2-a][1,4,7,10]tetraazacyclotridecin-3-yl]hexanamide
-
-
N-hydroxy-6-[4-(2-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(3-methylphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(4-methylphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(6-methoxynaphthalen-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-4-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(quinolin-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(quinolin-7-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(thiophen-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-{4-[4-(pyridin-4-yl)phenyl]-1H-1,2,3-triazol-1-yl}hexanamide
-
-
N-hydroxy-6-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}hexanamide
N-hydroxy-7-(4-phenyl-1H-1,2,3-triazol-1-yl)heptanamide
-
-
N-hydroxy-7-[(2E)-2-[(2-hydroxynaphthalen-1-yl)methylidene]hydrazino]-7-oxoheptanamide
-
N-hydroxy-7-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazino]-7-oxoheptanamide
-
N-hydroxy-7-[(2E)-2-[[4-(1H-imidazol-1-yl)phenyl]methylidene]hydrazino]-7-oxoheptanamide
-
N-hydroxy-7-[4-(6-methoxynaphthalen-2-yl)-1H-1,2,3-triazol-1-yl]heptanamide
-
-
N-hydroxy-7-[4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl]heptanamide
-
-
N-hydroxy-7-{4-[4-(pyridin-4-yl)phenyl]-1H-1,2,3-triazol-1-yl}heptanamide
-
-
N-hydroxy-7-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}heptanamide
N-hydroxy-8-oxo-8-[(2E)-2-[(2,4,6-trihydroxyphenyl)methylidene]hydrazino]octanamide
-
N-hydroxy-8-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}octanamide
N-hydroxy-N~3~-[5-(propan-2-yl)naphthalene-1-sulfonyl]-beta-alaninamide
N-hydroxynaphthalene-1-carboxamide
-
HDAC8-selective inhibitor
N-methyl-N-(quinoxalin-6-ylmethyl)-5-(trifluoroacetyl)thiophene-2-carboxamide
-
-
N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
-
-
N-[(2E)-3-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]prop-2-en-1-yl]-2-sulfanylacetamide
-
N-[(3E)-4-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl]-2-sulfanylacetamide
-
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N7-hydroxyheptanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0061 and 0.0122 microM, respectively
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N8-hydroxyoctanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00298 and 0.0091 microM, respectively
N1-hydroxy-N7-(5-phenyl-1,3,4-thiadiazol-2-yl)heptanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0055 and 0.0129 microM, respectively
N1-hydroxy-N8-(5-phenyl-1,3,4-thiadiazol-2-yl)octanediamide
-
-
N1-methyl-2-oxo-N9-phenylnonanediamide
-
-
NaCl
inhibitory in sodium phosphate/citric acid buffer, 50% inhibition at 100 mM
NVP-LAQ824
-
-
oxamflatin
-
p300
-
p300 can inactivate HDAC6 by acetylation
-
panobinostat
PAOA
-
-
PCI-24781
-
broad-spectrum or pan-HDAC inhibitor
PCI-34051
-
HDAC8-selective inhibitor
peroxynitrite
-
activity of wild-type enzyme is reduced to 38% in presence of peroxynitrite. Activities of mutants Y153A and Y253A are 233 completely abolished in the presence of peroxynitrite. Mutant Y146A shows 32% reduction in activity
phenyl butyric acid
-
-
phenylbutyrate
-
Buphenyl
phenylbutyric acid
-
-
Propionic acid
-
80% residual activity at 0.5 mM
PXD-101
PXD101
-
-
pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate
i.e. MS27-275
R306465
-
-
resminostat
romidepsin
S-(2-hydroxyethyl) methanesulfonothioate
-
-
S-nitrosocysteine
the activity of HDAC8 is significantly inhibited when incubated with S-nitrosoglutathione and S-nitrosocysteine in a time- and dosage-dependent manner. Sodium nitroprusside and dithiothreitol cannot reverse this inhibition
S-nitrosoglutathione
HDAC8 can be S-nitrosylated by S-nitrosoglutathione in vitro, and the activity of HDAC8 is significantly inhibited when incubated with S-nitrosoglutathione and S-nitrosocysteine in a time- and dosage-dependent manner. Sodium nitroprusside and dithiothreitol cannot reverse this inhibition
S-[2-[(2-propylpentanoyl)amino]ethyl]methanesulfonothioate
-
-
S-[7-oxo-7-(2-phenyl1,3-thiazol-5-ylamino)heptyl] 2-methylpropanethioate
-
analysis of growth inhibition of various cancer cells and comparison with suberoylanilide hydroxamic acid
SAHA
-
-
salicylic acid
-
92% residual activity at 0.5 mM
SB-939
-
-
scriptaid
-
-
SK7041
-
i.e. 4-dimethylamino-N-[4-(2-hydroxylcarbamoyl-vinyl)benzyl] benzamide
sodium butyrate
sodium phenylbutyrate
-
-
sorbic acid
-
91% residual activity at 0.5 mM
spiruchostatin
-
-
suberoyl anilide hydroxamic acid
-
-
suberoylanilide hydroxamic acid
suberoylanilide hydroxyamic acid
-
a specific inhibitor of zinc-dependent histone deacetylase activity. The compound directly induces p19INK4d expression in regenerating liver by increasing p19INK4d promoter-associated histone acetylation, molecular mechanisms by which the inhibitor delays liver regeneration exerting promoter-specific effects on histone acetylation during liver regeneration, overview
-
suberoylanilide trifluoromethylketone
sulforaphane
tartaric acid
-
90% residual activity at 0.5 mM
trapoxin A
-
-
trapoxin B
trichostatin A
trichostatin-A
troglitazone
-
-
tubacin
Valeric acid
-
83% residual activity at 0.5 mM
Valproate
-
class I-selective HDAC inhibitor
Valproic acid
vorinostat
[4-[(E)-[[6-(hydroxyamino)-6-oxohexanoyl]hydrazono]methyl]phenyl]boronic acid
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
heat shock protein 70
Hsp70
-
N-(cyclohexylcarbamothioyl)benzamide
-
10 microM, 5.6fold activation of HDAC8. No activation of other HDAC isoenzymes
N-(phenylcarbamothioyl)benzamide
-
10 microM, 12fold activation of HDAC8. No activation of other HDAC isoenzymes
N-[(3,5-dimethoxyphenyl)carbamothioyl]benzamide
-
10 microM, 8.4fold activation of HDAC8. No activation of other HDAC isoenzymes
additional information
-
in Tris/HCl buffer, optimum concentration of NaCl is 50 mM for isoforms HD1 and HD2 and 100 mM for the nuclear matrix form
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00244 - 0.01646
Ac-DQK(acetyl)-7-amido-4-methylcoumarin
0.00228 - 0.0359
Ac-FEK(acetyl)-7-amido-4-methylcoumarin
0.0043 - 0.0877
Ac-GGK(acetyl)-7-amido-4-methylcoumarin
0.0123 - 0.0666
Ac-GS(PO3)K(acetyl)-7-amido-4-methylcoumarin
0.00405 - 0.0241
Ac-GSK(acetyl)-7-amido-4-methylcoumarin
0.00069 - 0.108
Ac-IHK(acetyl)-7-amido-4-methylcoumarin
0.0124
Ac-ILK(acetyl)-7-amido-4-methylcoumarin
-
isoform HDAC3
0.0054
Ac-KGK(acetyl)-7-amido-4-methylcoumarin
-
isoform FB188 HDAH
0.019
Ac-KSK(acetyl)-7-amido-4-methylcoumarin
-
isoform FB188 HDAH
0.005
Ac-KWK(acetyl)-7-amido-4-methylcoumarin
-
isoform HDAC1
0.0044 - 0.107
Ac-KYK(acetyl)-7-amido-4-methylcoumarin
0.03
Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin
apparent KM
0.00303
Ac-LIK(acetyl)-7-amido-4-methylcoumarin
-
isoform HDAC1
0.0069 - 0.03
Ac-LYK(acetyl)-7-amido-4-methylcoumarin
0.01
Ac-PFK(acetyl)-7-amido-4-methylcoumarin
-
isoform HDAC8
0.0119 - 0.0221
Ac-VLK(acetyl)-7-amido-4-methylcoumarin
0.078 - 0.099
benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin
0.03 - 0.061
benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin
0.000015 - 0.0038
Fluor de Lys
0.013 - 0.088
Fluor de Lys HDAC substrate
0.14 - 1.1
Fluor de Lys HDAC8 substrate
0.16 - 1.1
RHK(acetyl)K(acetyl)-fluorophore
additional information
additional information
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.19
Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin
Plasmodium falciparum
Q7K6A1
-
0.0019 - 0.29
Fluor de Lys
0.0002 - 1.1
Fluor de Lys HDAC substrate
0.007 - 1.2
Fluor de Lys HDAC8 substrate
0.48 - 1.2
RHK(acetyl)K(acetyl)-fluorophore